GNE-8505
Based on 1 Customer Validation
GNE-8505 is an orally active, blood-brain barrier-permeable selective dual leucine zipper kinase (DLK) inhibitor. GNE-8505 has an IC50 of 0.144 μM for pJNK, and EC50 of 0.457 μM for DRG. GNE-8505 inhibits the DLK/JNK pathway, reduces stress-induced c-Jun phosphorylation levels, decreases neuronal death and suppresses axonal degeneration. GNE-8505 reduces phosphorylated c-Jun levels in the retina, spinal cord and brain tissues of mice. GNE-8505 is applicable to research related to Alzheimer's disease and amyotrophic lateral sclerosis (ALS).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.53%
- CAS 番号: 1620573-48-9
- 分子式: C21H24F3N5O
- 分子量:419.44
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
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Help & FAQs
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生物活性
Single administration of GNE-8505 (35 mg/kg) significantly reduces the number of phosphorylated c-Jun-positive cells in the spinal cord of SOD1G93A ALS mice at the middle stage of the disease[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6N (SOD1G93A transgenic line, 14-week-old, mid-disease stage)[2]
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Dosage:35 mg/kg
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Administration:single dose
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Result:Reduced the number of p-c-Jun-positive cells in lumbar spinal cord sections compared to vehicle-treated mice.
化学情報
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CAS 番号 1620573-48-9
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性状 Solid
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分子量 419.44
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分子式 C21H24F3N5O
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Color White to off-white
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SMILES
FC(F)(F)C1=CC(C2=NN(C([C@@H]3[C@]4([H])[C@@]3([H])CN(C5COC5)C4)=C2)CC6CC6)=CN=C1N
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (238.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (273 KB)
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取扱説明書 (2659 KB)
参考文献
[2]. Le Pichon CE, et al. Loss of dual leucine zipper kinase signaling is protective in animal models of neurodegenerative disease. Sci Transl Med. 2017;9(403):eaag0394. [Content Brief]
[3]. Siu M, et al. JW. Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration. J Med Chem. 2018 Sep 27;61(18):8078-8087. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3841 mL | 11.9207 mL | 23.8413 mL | 59.6033 mL |
| 5 mM | 0.4768 mL | 2.3841 mL | 4.7683 mL | 11.9207 mL | |
| 10 mM | 0.2384 mL | 1.1921 mL | 2.3841 mL | 5.9603 mL | |
| 15 mM | 0.1589 mL | 0.7947 mL | 1.5894 mL | 3.9736 mL | |
| 20 mM | 0.1192 mL | 0.5960 mL | 1.1921 mL | 2.9802 mL | |
| 25 mM | 0.0954 mL | 0.4768 mL | 0.9537 mL | 2.3841 mL | |
| 30 mM | 0.0795 mL | 0.3974 mL | 0.7947 mL | 1.9868 mL | |
| 40 mM | 0.0596 mL | 0.2980 mL | 0.5960 mL | 1.4901 mL | |
| 50 mM | 0.0477 mL | 0.2384 mL | 0.4768 mL | 1.1921 mL | |
| 60 mM | 0.0397 mL | 0.1987 mL | 0.3974 mL | 0.9934 mL | |
| 80 mM | 0.0298 mL | 0.1490 mL | 0.2980 mL | 0.7450 mL | |
| 100 mM | 0.0238 mL | 0.1192 mL | 0.2384 mL | 0.5960 mL |
GNE-8505 関連分類
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